Zaloglanstat (ISC-27864, GRC-27864)

Chemical Structure : Zaloglanstat

CAS No.: 1513852-12-4

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货号: PC-38688Not For Human Use, Lab Use Only.

Zaloglanstat (ISC-27864, GRC-27864) is a potent, selective, non-opioid and orally active microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor with IC50 of 5 nM (human mPGES-1).

规格	价格	库存
5 mg	￥2780	In stock
10 mg	￥4580	In stock
25 mg	￥7280	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

Zaloglanstat (ISC-27864, GRC-27864) is a potent, selective, non-opioid and orally active microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor with IC50 of 5 nM (human mPGES-1).

Zaloglanstat (ISC-27864, GRC-27864) shows no significant inhibitory effect on COX-1/2.

Zaloglanstat inhibits PGE2 release in pig and dog whole blood with IC50s of 161 nM and 154 nM, respectively.

Zaloglanstat blocks the conversion of arachidonic acid metabolite prostaglandin PGH2 to prostaglandin PGE2, thereby inhibiting inflammation-related PGE2 overproduction and reducing inflammatory responses and pain.

Zaloglanstat inhibits IL-1β-induced PGE2 release in A549 cells and human synovial fibroblasts in vitro.

Zaloglanstat exhibits significant analgesic efficacy in preclinical models for osteoarthritis and inflammatory arthritis.

物理化学性质&存储条件

分子量	452.862
分子式	C21H20ClF3N4O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(4-chloro-3-(5-oxo-1-(4-(trifluoromethyl)phenyl)-2,5-dihydro-1H-1,2,4-triazol-3-yl)benzyl)pivalamide

参考文献

1. Sant S, et al. Osteoarthritis Cartilage 2018, 26, S351– S352, DOI: 10.1016/j.joca.2018.02.698